Cat. No.: HY-109103

Tegatrabetan

(Synonyms: Tegavivint; BC2059)

6 Cited Publications

Customer Review

Based on 6 publication(s) in Google Scholar

Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).

For research use only. We do not sell to patients.

Purity: 99.84%
CAS No.: 1227637-23-1
Formula: C₂₈H₃₆N₄O₆S₂
Molecular Weight:588.74

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tegatrabetan Chemical Structure

CAS No.: 1227637-23-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (6)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1)^[1].

IC₅₀ & Target

β-Catenin^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.05169 μM Compound: 14, BC-2059	Growth inhibition of human A549 cells after 72 hrs by APH assay Growth inhibition of human A549 cells after 72 hrs by APH assay	[PMID: 26182238]
Cancer cell lines	IC₅₀	0.02001 μM Compound: 14, BC-2059	Cytotoxicity against human breast cancer cell aggregates grown on matrigel incubated for 72 hrs by MTS assay Cytotoxicity against human breast cancer cell aggregates grown on matrigel incubated for 72 hrs by MTS assay	[PMID: 26182238]
Cancer cell lines	IC₅₀	0.02075 μM Compound: 14, BC-2059	Cytotoxicity against human prostate cancer cells after 72 hrs by MTS assay Cytotoxicity against human prostate cancer cells after 72 hrs by MTS assay	[PMID: 26182238]
Cancer cell lines	IC₅₀	0.02992 μM Compound: 14, BC-2059	Cytotoxicity against human colon cancer cell aggregates grown on matrigel incubated for 72 hrs by MTS assay Cytotoxicity against human colon cancer cell aggregates grown on matrigel incubated for 72 hrs by MTS assay	[PMID: 26182238]
Cancer cell lines	IC₅₀	0.5305 μM Compound: 14, BC-2059	Cytotoxicity against human ovarian cancer cell aggregates grown on matrigel incubated for 72 hrs by MTS assay Cytotoxicity against human ovarian cancer cell aggregates grown on matrigel incubated for 72 hrs by MTS assay	[PMID: 26182238]
HCT-116	IC₅₀	0.02019 μM Compound: 14, BC-2059	Growth inhibition of human HCT116 cells after 72 hrs by APH assay Growth inhibition of human HCT116 cells after 72 hrs by APH assay	[PMID: 26182238]
HCT-15	IC₅₀	0.03057 μM Compound: 14, BC-2059	Growth inhibition of human HCT15 cells after 72 hrs by APH assay Growth inhibition of human HCT15 cells after 72 hrs by APH assay	[PMID: 26182238]
HCT-15	IC₅₀	0.03806 μM Compound: 14, BC-2059	Cytotoxicity against human HCT15 cell aggregates grown on matrigel incubated for 72 hrs by MTS assay Cytotoxicity against human HCT15 cell aggregates grown on matrigel incubated for 72 hrs by MTS assay	[PMID: 26182238]
HT-29	GI₅₀	0.09 μM Compound: 14, BC-2059	Growth inhibition of human HT-29 cells after 72 hrs by APH assay Growth inhibition of human HT-29 cells after 72 hrs by APH assay	[PMID: 26182238]
HT-29	IC₅₀	0.63 μM Compound: 14, BC-2059	Inhibition of Wnt/beta-catenin transcriptional activity in human HT-29 cells assessed as depletion of beta-catenin level by TCF luciferase promoter reporter assay Inhibition of Wnt/beta-catenin transcriptional activity in human HT-29 cells assessed as depletion of beta-catenin level by TCF luciferase promoter reporter assay	[PMID: 26182238]
MCF7	IC₅₀	0.08078 μM Compound: 14, BC-2059	Growth inhibition of human MCF7 cells after 72 hrs by APH assay Growth inhibition of human MCF7 cells after 72 hrs by APH assay	[PMID: 26182238]
SW480	IC₅₀	0.02329 μM Compound: 14, BC-2059	Growth inhibition of human SW480 cells after 72 hrs by APH assay Growth inhibition of human SW480 cells after 72 hrs by APH assay	[PMID: 26182238]

In Vitro

Tegatrabetan (BC2059; 20-100 nM; 48 hours) inhibits cell proliferation in suspension culture over 120 hours and induces apoptosis of cultured human acute myeloid leukemia (AML) HL-60, OCI-AML3 and MV4-11 cells dose-dependently^[1].
Tegatrabetan (20 and 50 nM; 24 hours) induces a modest but significant accumulation of cells in the G0/G1 phase, with a concomitant decline in the G2/M phase of the cell cycle^[1].
Tegatrabetan (100 nM, 24 hours) depletes the levels of β-catenin and its target genes, including c-MYC and survivin without affecting the levels of the TBL1 in OCI-AML3, HL-60 and MV4-11 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

HL-60, OCI-AML3 and MV4-11 cells
Concentration:

20, 50, and 100 nM
Incubation Time:

48 hours
Result:

Dose-dependently inhibited cell proliferation.

Cell Cycle Analysis^[1]

Cell Line:

OCI-AML3 cells
Concentration:

20 and 50 nM
Incubation Time:

24 hours
Result:

Dose-dependently induced cell cycle growth arrest.

Western Blot Analysis^[1]

Cell Line:

OCI-AML3, HL-60 and MV4-11 cells
Concentration:

100 nM
Incubation Time:

24 hours
Result:

Treatment depleted β-Catenin expression levels.

In Vivo

Tegatrabetan (BC2059; 1.0 or 5.0 mg/kg/day; intravenously) significantly improves the median survival of the mice from approximately 17.5 to 39 days. Treatment with Tegatrabetan (10 mg/kg/day; intravenously) alone further improves the median survival to 51.5 days^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NOD/SCID mice bearing OCI-AML3 xenografts^[1]
Dosage:

1 mg/kg; 5 mg/kg; 10 mg/kg
Administration:

Intravenously; 1 mg/kg daily 4 days per week or 5 mg/kg or 10 mg/kg of BC2059 twice per week (Tuesday and Thursday) for 3 weeks.
Result:

Treatment significantly improved survival of NOD/SCID mice bearing OCI-AML3 xenografts.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1227637-23-1
Appearance Solid
Molecular Weight 588.74
Formula C₂₈H₃₆N₄O₆S₂
Color White to light yellow
SMILES

O=S(C1=CC2=C(C=C1)/C(C3=CC=C(S(=O)(N4C[C@H](C)C[C@H](C)C4)=O)C=C3/C2=N\O)=N\O)(N5C[C@H](C)C[C@H](C)C5)=O
Synonyms

Tegavivint; BC2059
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (6)

All Cell Proliferation/Viability AssayIn Vivo Efficacy StudyCell Imaging/Staining

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Journal Impact Factor

Nat Chem Biol

Tegavivint triggers TECR-dependent nonapoptotic cancer cell death. [Abstract]

2025 May 26. PMID: 40419770

Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26. [Abstract]

Images of spheroids grown in ultralow attachment plates treated with Tegavivint (Tega) (5 μM), and quantification of spheroid viability was performed with CellTiter-Glo.

Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26. [Abstract]

Tegatrabetan (Tega) (10 mg/kg; i.p.; twice a week) enlonged time to tumor tripling of Foxn1nsup>u mouse xenograft tumor model.

Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26. [Abstract]

Tegatrabetan (Tega) (2.5 μM) were lethal to RNF43-mutant-HPAF-II^N.

Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26. [Abstract]

Tegatrabetan (Tega) (2.5 μM) were lethal to Capan-2 cells.

Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26. [Abstract]

Tegavivint (Tega) (10^-8-10^-5 M; 48 h) caused HT-1080N cell death.
Eur J Pharmacol

Verdiperstat attenuates acute lung injury by modulating MPO/μ-calpain/β-catenin signaling. [Abstract]

2022 Jun 5:924:174940. PMID: 35461824
J Cell Sci

Tbl1 promotes Wnt/β-catenin signaling-induced degradation of the Tcf7l1 protein in mouse ESCs. [Abstract]

2024 May 1;137(9):jcs261241. PMID: 38639717
bioRxiv

Dissecting Complex Interactions Between Ferroptosis and the Proteasome. [Abstract]

2026 Mar 30:2026.03.28.714855. PMID: 41959534
bioRxiv

Dyr726, a brain-penetrant inhibitor of PI3Kα, Type III receptor tyrosine kinases, and WNT signaling. [Abstract]

2025 Mar 29:2025.03.26.645490. PMID: 40196701
Res Sq

A clinical drug candidate that triggers non-apoptotic cancer cell death. [Abstract]

2025 Feb 11:rs.3.rs-4138879. PMID: 39989975

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (84.93 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6985 mL

8.4927 mL

16.9854 mL

5 mM

0.3397 mL

1.6985 mL

3.3971 mL

10 mM

0.1699 mL

0.8493 mL

1.6985 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (4.25 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.25 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Fiskus W, et al. Pre-clinical efficacy of combined therapy with novel β-catenin antagonist BC2059 and histone deacetylase inhibitor against AML cells. Leukemia. 2015 Jun;29(6):1267-78. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6985 mL	8.4927 mL	16.9854 mL	42.4636 mL
	5 mM	0.3397 mL	1.6985 mL	3.3971 mL	8.4927 mL
	10 mM	0.1699 mL	0.8493 mL	1.6985 mL	4.2464 mL
	15 mM	0.1132 mL	0.5662 mL	1.1324 mL	2.8309 mL
	20 mM	0.0849 mL	0.4246 mL	0.8493 mL	2.1232 mL
	25 mM	0.0679 mL	0.3397 mL	0.6794 mL	1.6985 mL
	30 mM	0.0566 mL	0.2831 mL	0.5662 mL	1.4155 mL
	40 mM	0.0425 mL	0.2123 mL	0.4246 mL	1.0616 mL
	50 mM	0.0340 mL	0.1699 mL	0.3397 mL	0.8493 mL
	60 mM	0.0283 mL	0.1415 mL	0.2831 mL	0.7077 mL
	80 mM	0.0212 mL	0.1062 mL	0.2123 mL	0.5308 mL

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Tegatrabetan

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Cytoskeleton Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Antihypertensive Compound Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Tegatrabetan

Biological Activity

Chemical Information

Publications (6)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tegatrabetan

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Cytoskeleton Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Antihypertensive Compound Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Tegatrabetan

Biological Activity

Chemical Information

Publications (6)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tegatrabetan Related Classifications

HY-109103 Related Classifications